Indomethacin SOPHARMA

Active material: Indomethacin
When ATH: M02AA23
CCF: NSAIDs for outdoor use
When CSF: 05.01.02
Manufacturer: SOPHARMA AD (Bulgaria)

Pharmaceutical form, composition and packaging

40 g – aluminum tuba (1) – packs cardboard.

6 PC. – PVC containers (1) – packs cardboard.

30 PC. – packings Valium planimetric (1) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES.

Pharmacological action

NSAIDs, indole acetic acid derivative. Anti-inflammatory, analgesic and antipyretic effect. The mechanism of action is associated with inhibition of the enzyme COX, which leads to inhibition of prostaglandin synthesis from arachidonic acid.

Inhibits platelet aggregation.

The introduction of oral and parenteral weakens pain, especially joint pain at rest and in motion, reduction of morning stiffness and swelling of joints, increase range of motion. The anti-inflammatory effect is the end of the first week of treatment.

When applied topically, relieves pain, reduces swelling and erythema.

When applied topically, Besides, It helps to reduce morning stiffness, increase range of motion.

Pharmacokinetics

After oral indomethacin is rapidly absorbed from the gastrointestinal tract. C_max plasma achieved through 2 no. It is metabolized in the liver. Undergoes enterohepatic recycling. Indomethacin determined in plasma as the unchanged substance and metabolite unbound – dezmetilnogo, desbenzoilnogo, desmethyl-dezbenzoilnogo.

T_1/2 is about 4.5 no. Excreted in the urine – 60% in the form of unchanged substance and metabolite, and faeces – 33% mainly as metabolites.

Testimony

For systemic use: articular syndrome (incl. rheumatoid arthritis, osteoarthritis, ankiloziruyushtiy spondylitis, gout), pain in the spine, neuralgia, mialgii, traumatic inflammation of soft tissues and joints, rheumatism, diffuse connective tissue disease, dysmenorrhoea. As an aid in infectious and inflammatory diseases of upper respiratory tract, adnexa, prostatitis, Clean.

For topical application,: prevention of inflammation in surgical interventions for cataract and anterior segment of the eye, inhibition of miosis during surgery.

For outdoor use: articular syndrome (incl. rheumatoid arthritis, osteoarthritis, ankiloziruyushtiy spondylitis, gout), pain in the spine, neuralgia, mialgii, traumatic inflammation of soft tissues and joints.

Dosage regimen

Establish individually, taking into account the severity of the disease. For adults when administered starting dose – by 25 mg 2-3 times / day. In case of insufficient clinical response dose increase to 50 mg 3 times / day. Sustained release dosage forms are used 1-2 times / day. The maximum daily dose: 200 mg.

Upon reaching the effect of treatment was continued for 4 weeks in the same or a reduced dose. With prolonged use of the daily dose should not exceed 75 mg. Take after a meal.

For the treatment of acute conditions or edema exacerbation of chronic process is introduced into / m 60 mg 1-2 times / day. The duration of the / m – 7-14 days. Then indomethacin administered orally or rectally for 50-100 mg 2 times / day, The maximum daily dose should not exceed 200 mg. For maintenance treatment for rectal use 50-100 mg 1 time / day at night.

For topical ophthalmic dosage frequency and duration of use are determined individually.

External used 2 times / day.

Side effect

From the digestive system: nausea, anorexia, vomiting, pain and discomfort in the abdomen, constipation or diarrhea, erosive and ulcerative lesions, bleeding or perforation of the gastrointestinal tract; rarely – stricture of the intestine, stomatitis, gastritis, flatulence, bleeding from the sigmoid colon or diverticular, jaundice, hepatitis.

From the central and peripheral nervous system: dizziness, headache, depression, feeling tired; rarely – alarm, fainting, drowsiness, convulsions, perifericheskaya neuropathy, muscular weakness, involuntary muscle movements, sleep disorders, mental disorders (depersonalization, psychotic episodes), paresthesia, dysarthria, parkinsonizm.

Cardio-vascular system: swelling, increased blood pressure, tachycardia, chest pain, arrhythmia, palpitation, hypotension, congestive heart failure, hematuria.

Allergic reactions: rarely – itch, hives, angiit, uzlovataya эritema, skin rash, exfoliative dermatitis, Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis, hair loss, acute respiratory distress, a sharp drop in blood pressure, anaphylactic reactions, angioedema, dyspnoea, bronchial asthma, pulmonary edema.

From the hematopoietic system: rarely – leukopenia, petechiae or ecchymosis, purpura, aplastic and hemolytic anemia, thrombocytopenia, ICE syndrome.

From the senses: rarely – violation of the definition of visual perception, diplopia, orbital and periorbital pain, tynnyt, hearing loss, deafness.

From the urinary system: rarely – proteinuria, nephrotic syndrome, interstitial nephritis, renal dysfunction renal failure.

Metabolism: rarely – giperglikemiâ, glycosuria, hyperkalemia.

Other: rarely – vaginal bleeding, tides, increased perspiration, nose bleed, and increase the tension of the mammary glands, gynecomastia.

Local reactions: in place of the / m in some cases – Education infiltration, abscess; when applied to the rectum may cause irritation of the mucous membrane of the rectum, tenesmus, exacerbation of chronic colitis.

When applied topically: itch, redness, rash at the site of application.

Contraindications

Hypersensitivity to indomethacin, erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirinovaâ triad”, violation of hematopoiesis, expressed human liver and / or kidney, severe chronic heart failure, hypertension, pancreatitis, III trimester of pregnancy, Children up to age 14 years; Rectal: proctitis, recent bleeding from the rectum.

Pregnancy and lactation

Indomethacin is contraindicated in the III trimester of pregnancy. In I and II trimesters, and during lactation (breast-feeding) not recommended.

Indomethacin in small amounts excreted in breast milk.

Cautions

To use caution in elderly patients, as well as liver diseases, kidney, GI history, dyspeptic symptoms with the time of use, hypertension, Heart Failure, immediately after major surgery, Parkinsonism, epilepsy.

When specifying a history of allergic reactions to NSAIDs used only in emergency cases.

The treatment requires systematic monitoring of liver and kidney function, peripheral blood.

Not recommended simultaneous application of acetylsalicylic acid and other NSAIDs.

Should not be used concurrently with indomethacin diflunizalom.

With simultaneous use of indomethacin with lithium should be borne in mind the possibility of the onset of symptoms of toxic action of lithium.

The local application should not be applied to the wound surface of skin, and avoid contact with eyes or mucous membranes.

Effects on ability to drive vehicles and management mechanisms

During the period of treatment should refrain from potentially hazardous activities, associated with the need to focus and increased speed of psychomotor reactions.

Drug Interactions

With simultaneous use of indomethacin can reduce the effects of saluretics, beta-blockers; proximity effect anticoagulants.

With simultaneous use of indomethacin and diflunisal there is a risk of severe bleeding from the gastrointestinal tract.

While the use of probenecid may increase the concentration of indomethacin in plasma.

Indomethacin may reduce the tubular secretion of methotrexate, which leads to increased toxicity.

In an application with NSAIDs increases the toxicity of cyclosporine.

Indomethacin at a dose of 50 mg 3 times / day increases the concentration of lithium in blood plasma and reduces the clearance of lithium from the body in patients with mental illness.

With simultaneous use of indomethacin with digoxin may increase the concentration of digoxin in the blood plasma and an increase in half-life of digoxin.